Nickel-Catalyzed Difluoromethylation of Arylboronic Acids with Bromodifluoromethane  

作　　者：Xia-Ping Fu Yu-Lan Xiao Xingang Zhang 

机构地区：[1]Key Laboratory of Organofluorine Chemistry, Center for Excellence in Molecular Synthesis, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, 345 Lingling Road, Shanghai 200032, China

出　　处：《Chinese Journal of Chemistry》2018年第2期143-146,共4页中国化学（英文版）

基　　金：This work was financially supported by the National Natural Science Foundation of China （Nos. 21425208, 21672238, 21332010, and 21421002）, the Strategic Priority Research Program of Chinese Academy of Sciences （No. XDB20000000）, and SIOC.

摘　　要：Although bromodifluoromethane （BrCF2H） is a simple and readily available fluorine source, direct formation of difluoromethylated arenes with BrCF2H has not been reported. Herein, we describe an efficient method to access difluoromethylated arenes through a nickel-catalyzed difluoromethylation of arylboronic acids with BrCF2H. The reaction exhibits high efficiency, good functional group tolerance and broad substrate scope, thus providing an efficient route for applications in drug discovery and development. Preliminary mechanistic studies reveal that a difluoromethyl radical is involved in the reaction.Although bromodifluoromethane （BrCF2H） is a simple and readily available fluorine source, direct formation of difluoromethylated arenes with BrCF2H has not been reported. Herein, we describe an efficient method to access difluoromethylated arenes through a nickel-catalyzed difluoromethylation of arylboronic acids with BrCF2H. The reaction exhibits high efficiency, good functional group tolerance and broad substrate scope, thus providing an efficient route for applications in drug discovery and development. Preliminary mechanistic studies reveal that a difluoromethyl radical is involved in the reaction.

关 键 词：arylboronic acids bromodifluoromethane CROSS-COUPLING DIFLUOROMETHYLATION NICKEL 

分 类 号：O643.36[理学—物理化学] O614.813[理学—化学]